The antidepressant fluoxetine blocks the human small conductance calcium-activated potassium channels SK1, SK2 and SK3.
Neurosci Lett
; 346(1-2): 85-8, 2003 Jul 31.
Article
en En
| MEDLINE
| ID: mdl-12850554
The effects of fluoxetine (Prozac) on the activity of human small-conductance calcium-activated potassium (SK) channels were investigated utilizing a functional fluorescence assay with bis-(1,3-dibutylbarbituric acid)trimethine oxonol (DiBAC(4)(3)). Fluoxetine blocked SK channels stably expressed in HEK 293 cells in a concentration-dependent manner displaying half-maximal inhibitory concentrations (IC(50)) of 9 microM for hSK1, 7 microM for hSK2 and 20 microM for hSK3. The block of hSK3 channels was confirmed by whole cell patch-clamp recordings of the recombinant cells and human TE 671 cells. Fluoxetine also inhibited [(125)I]apamin binding in a concentration-dependent manner displaying IC(50) values of 63 microM for hSK1, 148 microM for hSK2 and 295 microM for hSK3. These results provide new information concerning the mechanism of therapeutic and/or side effects of one of the most widely used antidepressant drugs.
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Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Canales de Potasio
/
Fluoxetina
/
Antidepresivos de Segunda Generación
/
Bloqueadores de los Canales de Potasio
Límite:
Humans
Idioma:
En
Revista:
Neurosci Lett
Año:
2003
Tipo del documento:
Article
País de afiliación:
Italia
Pais de publicación:
Irlanda